Method of providing pirfenidone therapy to a patient

Abstract

The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. The invention discloses an optimized dose escalation scheme that results in the patient having increased tolerance to adverse events associated with the administration of pirfenidone. The invention also discloses a starter pack that may be used in conjunction with the dose escalation scheme.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application Ser. No. 60 / 870,593, filed Dec. 18, 2006, the disclosure of which is incorporated by reference in its entirety.BACKGROUND[0002]1. Field of the Invention[0003]The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy.[0004]2. Description of the Related Art[0005]Pirfenidone is small drug molecule whose chemical name is 5-methyl-1-phenyl-2-(1H)-pyridone. It is a non-peptide synthetic molecule with a molecular weight of 185.23 Daltons. Its chemical elements are expressed as C12H11NO, and its structure and synthesis are known. Pirfenidone is manufactured commercially and being evaluated clinically as a broad-spectrum anti-fibrotic drug. Several pirfenidone Investigational New Drug Applications (INDs) are currently on file with the U.S. Food and Drug Administration. Phase II human investigations are on...

AI Technical Summary

Benefits of technology

[0011]The present invention overcomes the unmet clinical need by providing an improved, optimized dose escalation scheme for the administration of pirfenidone. The dose escalation scheme of the present invention provides pirfenidone in an amount such that the full maximum dosage is not reached for at least one week. In a preferred embodiment, the full maximum dosage of pirfenidone is not reached until about Day 15 of treatment. The method of the present invention allows for a maximum dosage of 2,403 mg of pirfenidone per day to be administered to a patient and also reduces the incidence of adverse events associated with the administration of pirfenidone by more accurately matching dose escalation with tolerance development in the patient. Indeed, it has been observed that even as the dosage escalates using the dosing escalation scheme described herein, adverse events, such as somnolence, decrease.

Problems solved by technology

Experimental reports also show that pirfenidone blocks the synthesis and release of excessive amounts of TNF-α from macrophages and other cells.

Many of these effects can interfere with everyday activities and quality of life.

There is significant reason to believe that the Azuma dose escalation does not optimally match the rate of dose escalation with the rate at which a patient develops sufficient tolerance to reduce the incidence of adverse events.

Indeed, it has been observed that even as the dosage escalates using the dosing escalation scheme described herein, adverse events, such as somnolence, decrease.

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